Pifatidine, Roxatidine acetate hydrochloride, Hoe-760, TZU-0460, Gastralgin, Roxit, Altat, Xarcin

盐酸罗沙替丁醋酸酯 醋酸罗沙替丁 Chemical Name: N-[3-[3-(1-Piperidinylmethyl)phenoxy]propyl]acetoxyacetamide hydrochloride
CAS No. 93793-83-0, 78628-28-1 (free base)
项目整合开发状态: Launched-1986
项目研究机构: Teikoku Hormone (Originator), Sumitomo Pharmaceuticals (Not Determined), Takeda (Not Determined), Aventis Pharma (Licensee), Wassermann (Licensee)
合成路线:The reductocondensation of piperidine (I) with 3-hydroxybenzaldehyde (II) by means of sodium borohydride in ethanol gives 3-(1-piperidylmethyl)phenol (III),which is then condensed with N-(3-bromopropyl)phthalimide (IV) by means of NaH in DMF yielding N-[3-[3-(1-piperidylmethyl)phenoxy]propyl]phthalimide (V).The hydrolysis of (V) with hydrazine in ethanol affords 3-[3-(1-piperidylmethyl)phenoxy]propylamine (VI),which is acylated with hydroxyacetic acid (VII) at 200 C giving N-[3-[3-(1-piperidylmethyl)phenoxy]propyl]hydroxyacetamide (VIII).Finally,this compound is acetylated with acetic anhydride at 100 C.